2. MAPK/ERK Pathway Autophagy
  3. p38 MAPK Autophagy Mitophagy
  4. Adezmapimod hydrochloride

Adezmapimod hydrochloride  (Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride)

Cat. No.: HY-10256A Purity: 98.97%
COA Handling Instructions

Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator.

For research use only. We do not sell to patients.

Adezmapimod hydrochloride Chemical Structure

Adezmapimod hydrochloride Chemical Structure

CAS No. : 869185-85-3

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Solution
10 mM * 1 mL in DMSO USD 45 In-stock
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Customer Review

Based on 410 publication(s) in Google Scholar

Other Forms of Adezmapimod hydrochloride:

Adezmapimod hydrochloride Related Antibodies

Top Publications Citing Use of Products

376 Publications Citing Use of MCE Adezmapimod hydrochloride

IF
WB
IHC

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomaterials. 2018 Aug;175:19-29.  [Abstract]

    Western blotting analysis showing the related protein expression (MHC, MyoD, p38α, phospho-p38α) of C2C12 myoblasts after incubated for 6 days in DM containing 40 μg/mL AuNPs and Au-AgNPs in the presence or absence of SB203580 (SB).

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: PLoS Biol. 2018 May 11;16(5):e2004225.  [Abstract]

    Representative western blots of p-CREB (Ser133) and UCP-1 in iWAT from C57BL/6J mice after 4 wk of SB203580 treatment. These mice are exposed to cold for 2 d before analysis.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184.  [Abstract]

    Representative immunoblots of total lysates from BV2 cells treated with MPP+or/and U0126 (10 μM), SP600125 (SP, 10 μM) and SB203580 (SB, 10 μM) using the antibodies against DICER.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163.  [Abstract]

    Cells are pretreated with SP600125 (20 μM), SB203580 (20 μM) or U0126 (20 μM) in presence or absence of KLA, then incubated with LPS (1 μg/mL) for certain time. Cell lysates are subjected to western blot.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein levels of IL-1β and TNF-α are sharply downregulated by the addition of inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein level of MMP-9 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-ERK1/2/ERK1/2 is notably reduced by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-JNK1&JNK1 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-p38&p38 is downregulated by inhibitors SB203580, SP600125, and U0126.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Front Immunol. 2018 Dec 7;9:2854.  [Abstract]

    Neutrophils are pretreated with inhibitor of p38 MAPK (SB203580) and ERK1/2 (U0126), and the cells are then incubated with either SS2 ZY05719 or PMA for 3 h. Immunofluorescence is performed.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Acta Physiol (Oxf). 2018 Feb;222(2).  [Abstract]

    P38 inhibitor SB203580 pretreatment also decreases p-HSP27 and MMP9 levels induced by MICAL2-overexpression.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.  [Abstract]

    HepG2 cells are pre-incubated with 20 µM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20µM) for 24 h.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2018 Aug 1;315(2):C225-C235.  [Abstract]

    Western blot analysis shows that inhibiting MAPK cannot completely reverse increased expression of RNF2 and CDDP resistance of OC cells.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5450-5467.  [Abstract]

    Treatment with SB203580 significantly abolishes siPlectin-stimulated p38 activation.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: FASEB J. 2019 Feb;33(2):2435-2450.  [Abstract]

    Bile acids (BAs) cause nuclear translocation of NF-kB p65, an effect that is abolished by SB203580.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Endod. 2018 May;44(5):751-758.  [Abstract]

    p38 MAPK inhibition enhances DPC-Exos–induced tube formation. (A) p38 MAPK activity is measured by detecting Phospho-p38 MAPK. The ratio between Phospho-p38 MAPK and the p38 MAPK band is used for quantification. (B) The effects of VEGF-A and KDR expression after p38 MAPK inhibitor SB203580 treatment on DPC-Exos-stimulated HUVECs.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Nov;119(10):8450-8459.  [Abstract]

    Western blot results show a reduction in phosphorylated p38 MAPK in ADSCs after treatment with 20 μM SB203580, 20 μM SP600125, or 20 μM PD98059 for 1 hour.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Dec 2.  [Abstract]

    Western analysis of protein expression in the treatment of miR-543 and SB 203580.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.  [Abstract]

    P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.  [Abstract]

    P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Dec;175(23):4338-4352.  [Abstract]

    Treatment of macrophages with inhibitor of p38 (SB203580) or JNK (SP600125) inhibits the synthesis of pro-IL-1β in ZFP91-overexpressing THP-1 cells.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(5):1779-1792.  [Abstract]

    Western blot bands of p38, phospho-p38, ZO-1, Clau-din-1, and Occludin. JNK inhibitor SP600125 and p38 inhibitor SB203580 are used.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cell Death Differ. 2017 Mar;24(3):492-499.  [Abstract]

    LPS stimulates ICER expression via p38-CREB pathway. Effect of MAPK and IKK inhibitors on LPS-induced CREB phosphorylation in peritoneal macrophages.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32.  [Abstract]

    Effects of p38 MAPK inhibitor (SB203580), ERK inhibitor (U0126), JNK inhibitor (SP600125), caspase inhibitor (Z-VAD-FMK) and NAC on SGC-7901 and MGC-803 treated with DOX/VCPA combination treatment. VCPA pretreatment strategy is the same as above. SB203580 (20 μM), U0126 (10 μM), SP600125 (20 μM), Z-VAD-FMK (10 μM) and NAC (5 mM) are treated 2 h before DOX (2 μg/mL) added into the culture, respectively. MAPK pathway protein levels are determined.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Nov;112:49-59.  [Abstract]

    Cells are pre-treated with ERK (U1026) and p38 (SB203580) inhibitors, followed by GL-V9 treatment for 24 h. Western blot is performed to analyze NAG-1 expression.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.  [Abstract]

    Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biochem Cell Biol. 2017 Feb;95(1):64-68.  [Abstract]

    The involvement of the p38 MAPK signaling pathways in lactoferrin-induced differentiation of HaCaT keratinocytes. HaCaT cells are differentiated in the presence or absence of 10 μM bovine Lactoferrin for 5 days. PD98059 (40 μM), SB203580 (10 μM), or LY294002 (10 μM) are added at the same time. Cell differentiation is evaluated by the expression levels of Involucrin and Filaggrin. GAPDH is used as a loading control.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

    Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(9):13542-13549.

    SB203580 decreases the expression ratio of p-p38 and p38 to inhibit activation of p38 MARK pathway.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.

    The Western blot analysis of HOG1 and Phospho-HOG1.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 19;8(60):101965-101983.  [Abstract]

    Representative western blot analysis of P-gp, p38 MAPK and phospho-p38 MAPK expression in MCF-7/MDR and K562/MDR cells treated with 10 μM SB203580 for 48 hr.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.  [Abstract]

    Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with SB203580 (a P38 inhibitor, 20 μM) for 1 h, followed by exposure to CPS (100 ng/mL) or MO (MOI = 30) for 48 h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: Chin Arch Otolaryngol Head Neck Surg. 2016,23(01):49-52.

    Effect of p38MAPK inhibitor on the soft palate reconstruction of the rats with chronic intermittent hypoxia.

    Adezmapimod hydrochloride purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79.  [Abstract]

    Dose response of MAPK and Akt inhibitors on cardiac fibroblast-derived exosomes (Exo)-induced activation of MAPKs and Akt. Neonatal rat cardiomyocytes are treated with or without Exo (50 μg/mL), U0126, SP600125, MK-2206, and SB023580 for 20 min and subjected to Western blot analysis. The results are from 4 separate experiments.

    View All p38 MAPK Isoform Specific Products:

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    p38 MAPK p38α p38β MAPK13 p38δ p38γ

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    Description

    Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator[1].

    IC50 & Target[1]

    p38

    50 nM (IC50)

    p38β2

    500 nM (IC50)

    In Vitro

    Adezmapimod hydrochloride (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM[1].
    ? Adezmapimod hydrochloride blocks PKB phosphorylation (IC50 3-5 μM). Adezmapimod hydrochloride inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Adezmapimod hydrochloride Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: CT6, BA/F3 cell line F7, and PBMC/T cells
    Concentration: 0-30 μM
    Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
    Result: Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM.

    Western Blot Analysis[1]

    Cell Line: CT6 cells, activated human T cells, and BA/F3 F7 cells
    Concentration: 0-30 μM
    Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
    Result: Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.
    In Vivo

    Adezmapimod hydrochloride (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors[1]
    Dosage: 5 mg/kg/day
    Administration: Intra peritoneal injected daily for 16 consecutive days
    Result: After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).  
    Molecular Weight

    413.90

    Appearance

    Solid

    Formula

    C21H17ClFN3OS
    CAS No.
    SMILES

    O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 years; -20°C, 6 months (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (241.60 mM; Need ultrasonic)

    H2O : 8.43 mg/mL (20.37 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4160 mL 12.0802 mL 24.1604 mL
    5 mM 0.4832 mL 2.4160 mL 4.8321 mL
    10 mM 0.2416 mL 1.2080 mL 2.4160 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.71%

    COA (253 KB) HNMR (167 KB) RP-HPLC (211 KB) LCMS (288 KB)

    Handling Instructions (2659 KB)
    References
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    Adezmapimod hydrochloride Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Adezmapimod869185-85-3SB 203580RWJ 64809SB203580SB-203580RWJ64809RWJ-64809p38 MAPKAutophagyMitophagyMitochondrial AutophagyATP-competitiveSAPK2aSAPK2bLCKGSK3βPKBαInhibitorinhibitorinhibit

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